Discovery of a Potent and Selective Inhibitor of Cyclin-Dependent Kinase 4/6 was written by Toogood, Peter L.;Harvey, Patricia J.;Repine, Joseph T.;Sheehan, Derek J.;VanderWel, Scott N.;Zhou, Hairong;Keller, Paul R.;McNamara, Dennis J.;Sherry, Debra;Zhu, Tong;Brodfuehrer, Joanne;Choi, Chung;Barvian, Mark R.;Fry, David W.. And the article was included in Journal of Medicinal Chemistry in 2005.Recommanded Product: 763-69-9 The following contents are mentioned in the article:
A pharmacol. approach to inhibition of cyclin-dependent kinases 4 and 6 (Cdk4/6) using highly selective small mol. inhibitors has the potential to provide novel cancer therapies for clin. use. Achieving high levels of selectivity for Cdk4/6, vs. other ATP-dependent kinases, presents a significant challenge. The pyrido[2,3-d]pyrimidin-7-one template provides an effective platform for the inhibition of a broad cross-section of kinases, including Cdks. It is now demonstrated that the modification of pyrido[2,3-d]pyrimidin-7-ones to include a 2-aminopyridine side chain at the C2-position provides inhibitors with exquisite selectivity for Cdk4/6 in vitro. This selectivity profile is recapitulated in cells where the most selective inhibitors create a G1 block at concentrations up to 100-fold the IC50 for cell proliferation. On the basis of its selectivity profile and pharmacokinetic profile, compound I (PD 0332991) was identified as a drug candidate for the treatment of cancer. This study involved multiple reactions and reactants, such as Ethyl 3-ethoxypropanoate (cas: 763-69-9Recommanded Product: 763-69-9).
Ethyl 3-ethoxypropanoate (cas: 763-69-9) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Esters contain a carbonyl center, which gives rise to 120° C–C–O and O–C–O angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C–O–C bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Recommanded Product: 763-69-9
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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics